ROR1-IN-4

ROR1-IN-4 is a selective ROR1 inhibitor with a Kd of 52 nM. ROR1-IN-4 shows potent anti-proliferative activity against TNBC cell line MDA-MB-231 (IC50 = 75 nM) . ROR1-IN-4 reduces colony formation, induces apoptosis and inhibits the phosphorylation of ROR1 (Tyr786) in MDA-MB-231 cells. ROR1-IN-4 demonstrates superior anti-tumor efficacy in nude mice bearing MDA-MB-231 subcutaneous xenografts. ROR1-IN-4 can be used for the study of triple-negative breast cancer (TNBC) [1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; Bcl-2 Family; PARP; ROR

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

FC(C1=CC(NC(C2=CC=C(C(C3=CC=C4N=C(N=CC4=C3)N)=C2)C)=O)=CC=C1CN5CCN(CC5)C)F

Molecular Formula

C29H30F2N6O

Molecular Weight

516.58

References & Citations

[1]Lu D, et al. Structure-Based Discovery of Quinazolin-2-amine Derivatives as Potent ROR1 Pseudokinase Inhibitors with In Vitro and In Vivo Efficacy against Triple-Negative Breast Cancer. J Med Chem. 2025 Aug 14;68 (15) :16138-16171.